{"entity":{"id":"enzalutamide","kind":"drug","name":"Enzalutamide","aka":[],"tldr":"Enzalutamide is a second-generation androgen-receptor blocker that stops the receptor binding testosterone, entering the nucleus and switching on genes. It is approved at every stage of advanced prostate cancer, from rising PSA after surgery to castration-resistant disease, and fatigue, falls and memory problems are its main drawbacks.","summary":"Enzalutamide is a second-generation androgen receptor antagonist that blocks ligand binding, nuclear translocation and DNA binding, giving more complete AR blockade than older antiandrogens. It is approved across every stage of advanced prostate cancer: AFFIRM and PREVAIL (mCRPC), PROSPER (nmCRPC), ARCHES and ENZAMET (mHSPC, overall survival benefit; ARCHES OS HR 0.66) and EMBARK (high-risk biochemical recurrence, 2023, metastasis-free survival HR 0.42 with leuprolide). It is the partner in TALAPRO-2 (talazoparib) and the MEVPRO trials (mevrometostat), so the next generation of combinations is built on it. Fatigue, falls and cognitive effects are the main toxicities, which is why darolutamide or apalutamide is sometimes preferred in frail men. For a newcomer, enzalutamide is the most widely used androgen-receptor blocker, from rising PSA after surgery to late-stage disease.","status":"approved","asOf":"2026-09-27","wikipedia":"https://en.wikipedia.org/wiki/Enzalutamide","links":[{"label":"FDA supplement approval letter: Xtandi NDA 203415/S-026 and NDA 213674/S-016 (EMBARK overall survival), 24 July 2026","url":"https://www.accessdata.fda.gov/drugsatfda_docs/appletter/2026/203415Orig1s026;213674Orig1s016ltr.pdf"},{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Enzalutamide"}],"tags":[],"related":[],"indications":["prostate","prostate-mhspc","prostate-nmcrpc","prostate-mcrpc","prostate-bcr"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":["pfizer"],"institutions":[],"pathways":[],"terms":["mcrpc-mhspc"],"trials":["embark","nct06520345","nct07611110"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Xtandi","modality":"Small-molecule AR antagonist","mechanism":"Second-generation AR antagonist blocking ligand binding, nuclear translocation, and DNA binding.","approvals":[{"region":"US","year":2012,"indication":"mCRPC after docetaxel (pre-chemo 2014)"},{"region":"US","year":2018,"indication":"Non-metastatic CRPC"},{"region":"US","year":2019,"indication":"mHSPC (ARCHES)"},{"region":"US","year":2023,"indication":"High-risk biochemical recurrence (EMBARK)"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[{"date":"2026-07-24","type":"label-change","region":"US","note":"US Prescribing Information updated with overall survival data from EMBARK (NDA 203415/S-026, NDA 213674/S-016; efficacy labelling change with clinical data)","source":"https://www.accessdata.fda.gov/drugsatfda_docs/appletter/2026/203415Orig1s026;213674Orig1s016ltr.pdf"}]},"route":"/drugs/enzalutamide/","neighbours":{"indication":[{"id":"prostate-bcr","kind":"indication","name":"Biochemical recurrence of prostate cancer","route":"/indications/prostate-bcr/"},{"id":"prostate-mcrpc","kind":"indication","name":"Metastatic castration-resistant prostate cancer","route":"/indications/prostate-mcrpc/"},{"id":"prostate-mhspc","kind":"indication","name":"Metastatic hormone-sensitive prostate cancer","route":"/indications/prostate-mhspc/"},{"id":"prostate-nmcrpc","kind":"indication","name":"Non-metastatic castration-resistant prostate cancer","route":"/indications/prostate-nmcrpc/"},{"id":"prostate","kind":"indication","name":"Prostate cancer","route":"/indications/prostate/"}],"company":[{"id":"pfizer","kind":"company","name":"Pfizer (incl. Seagen)","route":"/companies/pfizer/"}],"term":[{"id":"arpi","kind":"term","name":"Androgen receptor pathway inhibitor (ARPI)","route":"/terms/arpi/"},{"id":"mcrpc-mhspc","kind":"term","name":"mCRPC and mHSPC (castration-resistant vs hormone-sensitive prostate cancer)","route":"/terms/mcrpc-mhspc/"},{"id":"psa-kinetics","kind":"term","name":"PSA kinetics: PSA doubling time and PSA density","route":"/terms/psa-kinetics/"}],"trial":[{"id":"nct07226986","kind":"trial","name":"A Phase Ib/II Open-label Study of AMO959 With Lutetium (177Lu) Vipivotide Tetraxetan (AAA617) in Combination With ARPI in Adult Participants With PSMA","route":"/trials/nct07226986/"},{"id":"nct07611110","kind":"trial","name":"AZD2265 Compared With Standard of Care in PSMA-positive Metastatic Castration-resistant Prostate Cancer (VECTRA-01)","route":"/trials/nct07611110/"},{"id":"embark","kind":"trial","name":"EMBARK","route":"/trials/embark/"},{"id":"enza-p","kind":"trial","name":"ENZA-p","route":"/trials/enza-p/"},{"id":"prosper","kind":"trial","name":"PROSPER","route":"/trials/prosper/"},{"id":"stampede","kind":"trial","name":"STAMPEDE","route":"/trials/stampede/"},{"id":"nct06520345","kind":"trial","name":"The Study of 177Lu-TLX591 Plus SOC Versus SOC Alone in Patients With mCRPC (ProstACT Global)","route":"/trials/nct06520345/"}],"pathway":[{"id":"lineage-plasticity-neuroendocrine","kind":"pathway","name":"Lineage plasticity & neuroendocrine transformation","route":"/pathways/lineage-plasticity-neuroendocrine/"},{"id":"prostate-cancer-signalling","kind":"pathway","name":"Prostate cancer (KEGG map)","route":"/pathways/prostate-cancer-signalling/"}],"collection":[{"id":"prostate-cancer-foundation","kind":"collection","name":"Prostate Cancer Foundation (PCF)","route":"/collections/prostate-cancer-foundation/"}]}}